TW200745093A - Solid salt forms of a pyrrole substituted 2-indolinone - Google Patents

Solid salt forms of a pyrrole substituted 2-indolinone

Info

Publication number
TW200745093A
TW200745093A TW095134445A TW95134445A TW200745093A TW 200745093 A TW200745093 A TW 200745093A TW 095134445 A TW095134445 A TW 095134445A TW 95134445 A TW95134445 A TW 95134445A TW 200745093 A TW200745093 A TW 200745093A
Authority
TW
Taiwan
Prior art keywords
salt forms
indolinone
solid salt
pyrrole substituted
pyrrole
Prior art date
Application number
TW095134445A
Other languages
Chinese (zh)
Other versions
TWI310766B (en
Inventor
Changquan Calvin Sun
Michael Hawley
Original Assignee
Pfizer Prod Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of TW200745093A publication Critical patent/TW200745093A/en
Application granted granted Critical
Publication of TWI310766B publication Critical patent/TWI310766B/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

Abstract

The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pirrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.
TW095134445A 2005-09-19 2006-09-18 Solid salt forms of a pyrrole substituted 2-indolinone TWI310766B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US71858605P 2005-09-19 2005-09-19

Publications (2)

Publication Number Publication Date
TW200745093A true TW200745093A (en) 2007-12-16
TWI310766B TWI310766B (en) 2009-06-11

Family

ID=37626412

Family Applications (1)

Application Number Title Priority Date Filing Date
TW095134445A TWI310766B (en) 2005-09-19 2006-09-18 Solid salt forms of a pyrrole substituted 2-indolinone

Country Status (25)

Country Link
US (3) US20080275101A1 (en)
EP (2) EP1928858B1 (en)
JP (2) JP4519114B2 (en)
KR (1) KR101050906B1 (en)
CN (2) CN101287724B (en)
AR (1) AR056521A1 (en)
AU (1) AU2006293644B2 (en)
BR (1) BRPI0616374B8 (en)
CA (1) CA2621569C (en)
CY (1) CY1109326T1 (en)
DE (1) DE602006008015D1 (en)
DK (1) DK1928858T3 (en)
ES (1) ES2328407T3 (en)
HK (1) HK1125101A1 (en)
IL (1) IL189590A0 (en)
MX (1) MX2008002415A (en)
NO (1) NO20080866L (en)
NZ (1) NZ566033A (en)
PL (1) PL1928858T3 (en)
PT (1) PT1928858E (en)
RU (1) RU2399619C2 (en)
SI (1) SI1928858T1 (en)
TW (1) TWI310766B (en)
WO (1) WO2007034272A1 (en)
ZA (1) ZA200801431B (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1928858T1 (en) 2005-09-19 2009-10-31 Pfizer Prod Inc Solid salt forms of a pyrrole substituted 2-indolinone
US20100189791A1 (en) 2009-01-23 2010-07-29 Teva Pharmaceutical Industries, Ltd. Delayed release rasagiline malate formulation
EP2545034A1 (en) 2010-03-10 2013-01-16 Synthon B.V. A process for amidation of pyrrole carboxylate compounds

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6574293B1 (en) 1998-10-28 2003-06-03 Ericsson Inc. Receivers and methods for reducing interference in radio communications
US20020010203A1 (en) * 1999-12-22 2002-01-24 Ken Lipson Methods of modulating c-kit tyrosine protein kinase function with indolinone compounds
NZ520640A (en) * 2000-02-15 2005-04-29 Upjohn Co Pyrrole substituted 2-indolinone protein kinase inhibitors
US6797725B2 (en) * 2001-04-09 2004-09-28 Sugen, Inc. Prodrugs of a 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
PT3168218T (en) 2001-08-15 2019-01-11 Pharmacia & Upjohn Co Llc A crystal comprising an l-malic acid salt of n-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide for use as a medicament
US7119209B2 (en) * 2002-02-15 2006-10-10 Pharmacia & Upjohn Company Process for preparing indolinone derivatives
US7452913B2 (en) * 2003-02-24 2008-11-18 Pharmacia & Upjohn Company Polymorphs of pyrrole substituted 2-indolinone protein kinase inhibitors
US20040209937A1 (en) * 2003-02-24 2004-10-21 Sugen, Inc. Treatment of excessive osteolysis with indolinone compounds
US20060009510A1 (en) * 2004-07-09 2006-01-12 Pharmacia & Upjohn Company Llc Method of synthesizing indolinone compounds
SI1928858T1 (en) 2005-09-19 2009-10-31 Pfizer Prod Inc Solid salt forms of a pyrrole substituted 2-indolinone

Also Published As

Publication number Publication date
CN103601720B (en) 2016-08-10
EP1928858A1 (en) 2008-06-11
CA2621569C (en) 2010-10-19
AU2006293644B2 (en) 2012-05-31
PT1928858E (en) 2009-09-17
CN103601720A (en) 2014-02-26
NO20080866L (en) 2008-03-13
WO2007034272A1 (en) 2007-03-29
AR056521A1 (en) 2007-10-10
RU2008109959A (en) 2009-10-27
AU2006293644A1 (en) 2007-03-29
CN101287724B (en) 2013-11-06
CA2621569A1 (en) 2007-03-29
NZ566033A (en) 2011-04-29
CY1109326T1 (en) 2014-07-02
SI1928858T1 (en) 2009-10-31
ZA200801431B (en) 2009-07-29
US20150158849A1 (en) 2015-06-11
BRPI0616374A2 (en) 2011-06-21
PL1928858T3 (en) 2009-12-31
US20120142749A1 (en) 2012-06-07
JP2007084540A (en) 2007-04-05
JP4519114B2 (en) 2010-08-04
MX2008002415A (en) 2008-03-27
EP1928858B1 (en) 2009-07-22
TWI310766B (en) 2009-06-11
HK1125101A1 (en) 2009-07-31
US20080275101A1 (en) 2008-11-06
BRPI0616374B8 (en) 2021-05-25
RU2399619C2 (en) 2010-09-20
DE602006008015D1 (en) 2009-09-03
IL189590A0 (en) 2008-08-07
KR101050906B1 (en) 2011-07-20
KR20080037093A (en) 2008-04-29
US8987320B2 (en) 2015-03-24
ES2328407T3 (en) 2009-11-12
JP2010090152A (en) 2010-04-22
BRPI0616374B1 (en) 2020-05-12
CN101287724A (en) 2008-10-15
EP2112148A1 (en) 2009-10-28
DK1928858T3 (en) 2009-10-26
US9290479B2 (en) 2016-03-22

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